HUP0003962A2 - Kinuklidinil-származékok, eljárás előállításukra, e vegyületeket tartalmazó gyógyászati készítmények, e vegyületek alkalmazása, valamint intermedierjeik - Google Patents
Kinuklidinil-származékok, eljárás előállításukra, e vegyületeket tartalmazó gyógyászati készítmények, e vegyületek alkalmazása, valamint intermedierjeikInfo
- Publication number
- HUP0003962A2 HUP0003962A2 HU0003962A HUP0003962A HUP0003962A2 HU P0003962 A2 HUP0003962 A2 HU P0003962A2 HU 0003962 A HU0003962 A HU 0003962A HU P0003962 A HUP0003962 A HU P0003962A HU P0003962 A2 HUP0003962 A2 HU P0003962A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- substituted
- alkyl
- cycloalkyl
- thienyl
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical class C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 1
- 108010040722 Neurokinin-2 Receptors Proteins 0.000 abstract 1
- 102100037342 Substance-K receptor Human genes 0.000 abstract 1
- 102100037346 Substance-P receptor Human genes 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 150000001450 anions Chemical class 0.000 abstract 1
- 125000005605 benzo group Chemical group 0.000 abstract 1
- -1 benzo[b]thienyl Chemical group 0.000 abstract 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P27/00—Drugs for disorders of the senses
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Abstract
A találmány szerinti vegyületek NK1 és NK2 receptor-antagonista (I)általános képletében R jelentése fenilcsoport, cikloalkilcsoport vagy heteroarilcsoport,amelyek benzocsoporttal vagy cikloalkilcsoporttal kondenzáltak éshelyettesítettek lehetnek, ahol a helyettesítők (helyettesített)alkilcsoport, (helyettesített) alkoxicsoport, fenoxicsoport,alkanoilcsoport, halogénatom, alkoxi-karbonil-csoport,cikloalkilcsoport, -S(O)m-alkil-csoport, cianocsoport, -NR2R3, -S(O)mNR2R3, -NR4 alkanoilcsoport és -CONR2R3 általános képletű csoportlehetnek, vagy R 2,3-dihidrobenzo[b]furanil- vagy kromanilcsoportotjelent; R1, R2, R3 és R4 jelentése egymástól függetlenül hidrogénatom vagyalkilcsoport, vagy R2 és R3 együtt alkiléncsoportot képeznek; W jelentése kovalens kötés vagy metilén-, vagy etiléncsoport; X jelentése alkiléncsoport; Y jelentése fenilcsoport, naftilcsoport, benzilcsoport,piridilcsoport, tienilcsoport vagy cikloalkilcsoport, amelyekhelyettesítettek lehetnek, ahol a helyettesítők alkilcsoport,alkoxicsoport, fluoratommal helyettesített alkil- vagy alkoxicsoport,halogénatom és cianocsoport lehetnek; Ar jelentése fenil-, naftil-, benzil-, tienil-, benzo[b]tienil- vagyindolilcsoport, amelyek helyettesítettek lehetnek, és a helyettesítők(helyettesített) alkilcsoport, (helyettesített) alkoxicsoport,halogénatom és cianocsoport lehetnek, vagy Ar 1,3-benzodioxolán-4-vagy -5-il- vagy 1,4-benzodioxán-5- vagy -6-il-csoportot jelent; m értéke 0, 1 vagy 2; és ZA gyógyászatilag elfogadható aniont jelent. A találmány tárgyköréheztartoznak továbbá a fenti vegyületek előállítása, e vegyületekettartalmazó gyógyászati készítmények, e vegyületek alkalmazása ésintermedierjeik. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9712882.1A GB9712882D0 (en) | 1997-06-18 | 1997-06-18 | Quaternary ammonium compounds |
| PCT/EP1998/003500 WO1998057972A1 (en) | 1997-06-18 | 1998-06-05 | Quaternary ammonium compounds as tachykinin antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0003962A2 true HUP0003962A2 (hu) | 2001-04-28 |
| HUP0003962A3 HUP0003962A3 (en) | 2001-12-28 |
Family
ID=10814535
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0003962A HUP0003962A3 (en) | 1997-06-18 | 1998-06-05 | Quinuclidinium compounds process for preparing thereof, pharmaceutical compositions comprising thereof, their use, and their intermediates |
Country Status (43)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999033491A1 (fr) * | 1997-12-26 | 1999-07-08 | Yamanouchi Pharmaceutical Co., Ltd. | Compositions medicinales a liberation prolongee |
| JP4546589B2 (ja) * | 1998-04-23 | 2010-09-15 | 武田薬品工業株式会社 | ナフタレン誘導体 |
| ATE367811T1 (de) * | 2000-06-12 | 2007-08-15 | Univ Rochester | Methode zur behandlung von hitzewallungen, durch verwendung eines tachikinin-rezeptor antagonisten |
| WO2002046156A2 (en) * | 2000-12-06 | 2002-06-13 | Sepracor, Inc. | 4,4-disubstituted piperidines for use as dopamine, serotonin and norepinephrine ligands |
| AU2003243353A1 (en) * | 2002-05-29 | 2003-12-19 | The Regents Of The University Of California | Antagonizing nk1 receptors inhibits consumption of substances of abuse |
| WO2004091597A2 (en) * | 2003-04-15 | 2004-10-28 | Pharmacia & Upjohn Company Llc | Method of treating irritable bowel syndrome (ibs) |
| CN1980896A (zh) * | 2004-05-07 | 2007-06-13 | 詹森药业有限公司 | 咪唑衍生物的可放大合成 |
| EP2129381A1 (en) | 2007-01-24 | 2009-12-09 | Glaxo Group Limited | Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3991201A (en) * | 1974-06-27 | 1976-11-09 | Janssen Pharmaceutica N.V. | 1-(β-Aryl-β-R-ethyl)imidazoles as antimicrobial agents |
| US5583134A (en) * | 1992-09-30 | 1996-12-10 | Sanofi | 1-azoniabicyclo[2.2.2] octanes and pharmaceutical compositions in which they are present |
| FR2696178B1 (fr) * | 1992-09-30 | 1994-12-30 | Sanofi Elf | Amides basiques quaternaires, procédé pour leur préparation et compositions pharmaceutiques en contenant. |
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1997
- 1997-06-18 GB GBGB9712882.1A patent/GB9712882D0/en active Pending
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1998
- 1998-05-06 UA UA99126551A patent/UA62966C2/uk unknown
- 1998-05-19 TW TW087107720A patent/TW479055B/zh not_active IP Right Cessation
- 1998-06-04 HN HN1998000087A patent/HN1998000087A/es unknown
- 1998-06-04 PA PA19988452501A patent/PA8452501A1/es unknown
- 1998-06-05 NZ NZ501286A patent/NZ501286A/xx unknown
- 1998-06-05 AU AU82153/98A patent/AU726027B2/en not_active Ceased
- 1998-06-05 KR KR1019997011931A patent/KR100345389B1/ko not_active IP Right Cessation
- 1998-06-05 PL PL98337713A patent/PL189557B1/pl not_active IP Right Cessation
- 1998-06-05 HU HU0003962A patent/HUP0003962A3/hu unknown
- 1998-06-05 AT AT98932148T patent/ATE275564T1/de not_active IP Right Cessation
- 1998-06-05 BR BR9810619-8A patent/BR9810619A/pt not_active Application Discontinuation
- 1998-06-05 WO PCT/EP1998/003500 patent/WO1998057972A1/en not_active Application Discontinuation
- 1998-06-05 CN CNB988063425A patent/CN1199971C/zh not_active Expired - Fee Related
- 1998-06-05 EA EA199900986A patent/EA002424B1/ru not_active IP Right Cessation
- 1998-06-05 PT PT98932148T patent/PT994876E/pt unknown
- 1998-06-05 SK SK1744-99A patent/SK283346B6/sk unknown
- 1998-06-05 CA CA002291975A patent/CA2291975C/en not_active Expired - Fee Related
- 1998-06-05 IL IL13307998A patent/IL133079A/en not_active IP Right Cessation
- 1998-06-05 DE DE69826129T patent/DE69826129T2/de not_active Expired - Fee Related
- 1998-06-05 YU YU64699A patent/YU64699A/sh unknown
- 1998-06-05 IL IL15562198A patent/IL155621A0/xx not_active IP Right Cessation
- 1998-06-05 ID IDW991633A patent/ID23410A/id unknown
- 1998-06-05 SI SI9830692T patent/SI0994876T1/xx unknown
- 1998-06-05 JP JP50368799A patent/JP3280993B2/ja not_active Expired - Fee Related
- 1998-06-05 TR TR1999/03135T patent/TR199903135T2/xx unknown
- 1998-06-05 ES ES98932148T patent/ES2227856T3/es not_active Expired - Lifetime
- 1998-06-05 US US09/380,370 patent/US6207678B1/en not_active Expired - Fee Related
- 1998-06-05 EP EP98932148A patent/EP0994876B1/en not_active Expired - Lifetime
- 1998-06-08 PE PE1998000468A patent/PE80099A1/es not_active Application Discontinuation
- 1998-06-11 AP APAP/P/1998/001262A patent/AP947A/en active
- 1998-06-15 UY UY25045A patent/UY25045A1/es unknown
- 1998-06-16 MY MYPI98002689A patent/MY136376A/en unknown
- 1998-06-16 AR ARP980102853A patent/AR012249A1/es active IP Right Grant
- 1998-06-17 TN TNTNSN98089A patent/TNSN98089A1/fr unknown
- 1998-06-17 ZA ZA9805239A patent/ZA985239B/xx unknown
- 1998-06-17 DZ DZ980134A patent/DZ2524A1/xx active
- 1998-06-17 MA MA25118A patent/MA26509A1/fr unknown
- 1998-06-18 HR HR980337A patent/HRP980337B1/xx not_active IP Right Cessation
- 1998-06-18 CO CO98034807A patent/CO4940478A1/es unknown
-
1999
- 1999-11-23 IS IS5269A patent/IS5269A/is unknown
- 1999-11-23 BG BG103919A patent/BG63341B1/bg unknown
- 1999-11-25 NO NO995782A patent/NO995782L/no not_active Application Discontinuation
- 1999-12-15 OA OA9900281A patent/OA11235A/en unknown
-
2000
- 2000-12-11 US US09/734,266 patent/US6380396B1/en not_active Expired - Fee Related
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